A Rhodium(III)-Based Inhibitor of Lysine-Specific Histone Demethylase 1 as an Epigenetic Modulator in Prostate Cancer Cells

We
report herein a novel rhodium­(III) complex 1 as
a new LSD1 targeting agent and epigenetic modulator. Complex 1 disrupted the interaction of LSD1-H3K4me2 in human prostate
carcinoma cells and enhanced the amplification of p21, FOXA2, and
BMP2 gene promoters. Complex 1 was selective for LSD1
over other histone demethylases, such as KDM2b, KDM7, and MAO activities,
and also showed antiproliferative activity toward human cancer cells.
To date, complex 1 is the first metal-based inhibitor
of LSD1 activity.